Abstract: Disclosed are a sustained-release lipid composition and a preparation method therefore. Specifically, the present invention relates to a solid composition containing lipids and a liposome composition obtained therefrom, wherein the liposomes have improved release properties.
Abstract: Provided is a preparation method for a tyrosine kinase inhibitor and an intermediate thereof. Specifically, a preparation method for a cyanoquinoline compound is provided. The method has a high yield, good product purity, and mild reaction conditions.
Abstract: Disclosed is a method for preparing a benzofuran derivative. In particular, provided is a method for preparing a benzofuran derivative, wherein according to the method provided, reaction steps required to synthesize the benzofuran substance in the prior art can be effectively shortened.
Abstract: The present invention provides a human PD-1 antibody, an antigen-binding fragment thereof, and medical use thereof, and further provides a chimeric antibody and humanized antibodies comprising a complementarity-determining region (CDR) of the antibody, a pharmaceutical composition comprising the human PD-1 antibody and the antigen-binding fragment thereof, and use of the antibody in preparing medicines for treating diseases or disorders.
Abstract: Provided are an IL-5 antibody, an antigen binding fragment thereof, and a medical application therefor. The present invention comprises a mouse-derived antibody containing an IL-5 antibody CDR region, a chimeric antibody, a humanized antibody, and a pharmaceutical composition comprising said IL-5 antibody and said antigen binding fragment thereof, as well as the use of the pharmaceutical composition as a drug.
Abstract: A novel PD-L1 antibody, an antigen-binding fragment thereof, and a pharmaceutical use thereof. A humanized antibody comprising a CDR of the PD-L1 antibody, a pharmaceutical composition comprising the PD-L1 antibody and the antigen-binding fragment thereof and a use of the PD-L1 antibody as a drug. A use of a humanized PD-L1 antibody in preparing a drug for treating diseases or disorders associated with PD-L1.
Abstract: A preparation method for a compound represented by formula I or a pharmaceutically acceptable salt thereof, The method includes a step of reacting a compound represented by formula II with an inorganic or organic acid selected from the group consisting of hydrochloric acid, phosphoric acid and maleic acid to provide a compound represented by formula II? In the above formulas II and II?, R1 may be trifluoromethyl; and X may be hydrochloric acid, phosphoric acid, or maleic acid. The method also includes a step of reacting the compound represented by formula II? with a compound represented by formula IV: to provide the compound represented by formula I, wherein Ra is selected from hydroxyl, halogen or alkoxy.
Abstract: A TIM-3 antibody, an antigen-binding fragment thereof, and medical uses thereof are described. More specifically, the present invention provides a rat-derived antibody containing a CDR region of the TIM-3 antibody, a chimeric antibody or a human-derived antibody thereof, and a pharmaceutical composition containing the TIM-3 antibody and the antigen-binding fragment thereof, as well as uses thereof serving as a drug. In particular, the present invention provides uses of a human-derived TIM-3 antibody in the preparation of drugs for treating TIM-3-related conditions.
Abstract: This application discloses CD73 inhibitors represented by the general formula (I) and analogs thereof, pharmaceutical compositions containing these compounds, methods of preparing them, and use of these compounds as therapeutic agents for the treatment of diseases or conditions associated with CD73 activity, such as various cancers.
Abstract: The present disclosure relates to use of a composition containing a CDK4/6 inhibitor in combination with anastrozole in preparation of a medicament for treating tumor diseases. Specifically, the CDK4/6 inhibitor involved in the application is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
Abstract: A heteroaryl[4,3-c]pyrimidin-5-amine derivative, a preparation method therefor, and medical uses thereof are provided. Specifically, a heteroaryl[4,3-c]pyrimidin-5-amine derivative of formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and uses thereof as therapeutic agents are provided. In particular, the provided compounds can be used as A2a receptor antagonists and for treatment of conditions or symptoms that are ameliorated by inhibiting the A2a receptor. The various substituent groups in the formula (I) have the meanings as described in the specification.
Abstract: The present invention relates to a method for preparing a pyrimidone heteroaryl derivative and an intermediate of the pyrimidone heteroaryl derivative. Specifically, the pyrimidone heteroaryl derivative of the formula is prepared by changing a starting raw material and an intermediate.
Abstract: A solid dispersion, a method for preparing same, and a solid preparation including the solid dispersion. The solid dispersion contains (R)-4-amino-1-(1-(but-2-ynylacyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazine-7-one or a pharmaceutically acceptable salt thereof, and a carrier material. The carrier material is selected from hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate.
Abstract: Provided are a crystal form of an oxopicolinamide derivative and a preparation method therefor. In particular, provided are crystal forms A, B, C, D, E, and F of a compound as shown in formula (I) and a preparation method therefor. Crystal forms A, B, C, D, E, and F of the compound of formula (I) obtained in the present disclosure have good crystal stability and chemical stability, and can be better used in clinical treatment.
Type:
Grant
Filed:
February 26, 2019
Date of Patent:
April 12, 2022
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Junran Yang, Lin Wang, Qiyun Shao, Zhenxing Du, Likun Wang
Abstract: The present invention provides a crystal form of a 1,2,3-triazolo[1,5-a]pyrazines derivative and a preparation method for the crystal form. Specifically, the present invention provides a crystal form of a compound (S)-N5-(3,4-difluorophenyl)-6-methyl-N3-((R)-1,1,1-trifluoropropan-2-yl)-6,7-dihydro-[1,2,3]triazolo[1,5-c]pyrazine-3,5(4H)-dimethylformamide and a preparation method for the crystal form. The prepared crystal form has good stability and clinical application value.
Abstract: The present disclosure relates to a pharmaceutical composition, which comprises an IL-15 protein complex and a citrate buffer solution. In addition, the pharmaceutical composition may also comprise a sugar and a non-ionic surfactant. The pharmaceutical composition in the present disclosure demonstrates a high degree of stability even after being stored at 2-8° C. for several months.
Abstract: The present invention provides a fusion protein containing TGF-? receptor and pharmaceutical use thereof. Further, the present invention provides a bifunctional fusion protein comprising the PD-L1 antibody targeting portion and the TGF-?RII extracellular domain, and a pharmaceutical composition comprising the fusion protein containing TGF-? receptor, and the use thereof in the preparation of anti-cancer drug.
Abstract: The present invention relates to a piperazine heteroaryl derivative, a preparation method therefor and the use of same in medicine. In particular, the present invention relates to the piperazine heteroaryl derivative as shown in the general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and the use of same as a capsid protein inhibitor, in particular in the prevention and/or treatment of diseases such as hepatitis B, influenza, herpes, AIDS, etc. The definitions of each group in the general formula (I) are the same as those defined in the description.
Abstract: A pharmaceutical composition for topical administration and a preparation method therefor are described. In particular, a pharmaceutical composition comprising (3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide, or a pharmaceutically acceptable salt thereof, and diethylene glycol monoethyl ether is described.
Abstract: The present invention relates to crystal forms of an oxypyridine amide derivative and a preparation method therefor. In particular, the present invention relates to crystal forms A, B, C, D, E and F of a compound represented by formula (I) and a preparation method therefor. The crystal forms of the compound represented by formula (I) as described in the present invention have good crystal form stability and may be better for clinical use.